Design and synthesis of novel photoaffinity reagents for labeling VEGF receptor tyrosine kinases |
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Authors: | Sun-Young Han Bum Tae Kim |
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Institution: | Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea |
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Abstract: | Novel biotin-tagged photoaffinity probes based on a trifunctional tertiary amine scaffold were synthesized and evaluated as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. Probes 3a-c inhibit VEGF induced proliferation in HUVE cells, with IC50 values of 29.7, 33.3, and 37.7 μM, respectively. Moreover, we identified the interaction of 3b with VEGFR-2 in photoaffinity labeling experiment using HUVE cells. |
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Keywords: | Biotin-tagged photoaffinity probe Vascular endothelial growth factor receptors Ligand-receptor interactions Inhibitor Trifunctional probe |
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